GlmU-IN-1

GlmU-IN-1 is an inhibitor of the GlmU acetyltransferase domain in Escherichia coli and Haemophilus influenzae. GlmU-IN-1 acts as a competitive inhibitor of AcCoA and a non-competitive inhibitor of GlcN-1-P. GlmU-IN-1 targets the acetyltransferase domain of bacterial GlmU, interferes with the biosynthesis of UDP‑GlcNAc, and impairs bacterial cell wall integrity. GlmU-IN-1 can be used for the research of Gram-negative bacterial infections^[1]. In Vitro:GlmU-IN-1 (5175178) (0.39-100 μM; 30 min) potently and specifically inhibits the acetyltransferase activity of purified E. coli GlmU with an IC₅₀ of 1.40 μM, and inhibits the acetyltransferase activity of purified H. influenzae GlmU with an IC₅₀ of 79.92 μM. It acts as a competitive inhibitor against AcCoA and a non-competitive inhibitor against GlcN-1-P^[1].
GlmU-IN-1 (4 μg/mL; 30 min) disrupts the cell membrane permeability of E. coli ATCC 25922^[1].
GlmU-IN-1 (24 h) shows no cytotoxicity against HepG2 cells, with its CC₅₀ >150 μg/mL^[1].
GlmU-IN-1 (0.0625-32 μg/mL; 24 h) exhibits bactericidal activity against E. coli ATCC 25922 (MIC 4 μg/mL, MBC 32 μg/mL), and also shows antibacterial activity against NDM1-producing A. baumanii and K. pneumoniae isolates^[1].
GlmU-IN-1 inhibits the growth of E. coli BL21 (DE3) by targeting GlmU. Compared with wild-type and empty vector control cells, the bacterial IC₅₀ of GlmU-overexpressing cells is four times higher^[1].